Mucoadhesive buccal patches of lornoxicam: II- in-vivo evaluation and clinical efficacy

Lornoxicam is a NSAID of the oxicam class and it has the same side effects of this group when taken orally. In attempts to avoid the systemic side effects of lornoxicam [e.g. gastric irritation] and to achieve sustained release of the drug, several buccal patch formulations containing lornoxicam were prepared using different polymers and were evaluated for in-vitro characteristics in part I of this study. In the current study, the selected formulations [based on the previous in-vitro data] are evaluated for in-vivo performance using experimental animals and clinical efficacy on human volunteers. Pharmacokinetic parameters were assessed following application of the selected patches in rabbits. A comparative clinical study was conducted on patients with post-operative pain and edema following maxillofacial operations. The results of the in-vivo animal experiment showed that lornoxicam formulated in different buccal patches was successfully delivered to the systemic circulation and showed high absolute bioavailability of lornoxicam. The clinical study results revealed that sodium carboxy methyl cellulose [NaCMC, 3%] formulation applied to the buccal mucosa was slightly better or equally effective to the orally administered commercial oxicam product [Feldene Flash tablets] in reducing pain level, swelling and tenderness within a period of 4 days with no observed side effects. These findings suggest that lornoxicam administered in this buccal patch may present a potential therapeutic use as a strong anti-inflammatory and analgesic agent

Mucoadhesive buccal patches of lornoxicam: 1-development and in-vitro characterization

Lornoxicam as a non-steroidal anti-inflammatory drug [NSAID] has the same side effects of this group if taken orally [GIT, renal, and hepatic disorders]. Lornoxicam and its metabolites bind extensively to plasma albumin [99%], beside that, it has a relatively short half-life [3 to 5 hrs]. The drug was formulated in mucoadhesive buccal patches using different polymers including, hydroxyethyl cellulose [HEC], hydroxypropyl cellulose [HPC], hydroxypropylmethyl cellulose [HPMC], chitosan, polyvinyl alcohol [PVA,], gelatin, sodium alginate and sodium carboxymethyl cellulose [Na CMC]. The physical characteristics of the formulated patches as mass uniformity, patch thickness, surface pH, folding endurance, swelling, residence time as well as mucoadhesion [in-vitro and ex-vivo mucoadhesion force] were evaluated. The in-vitro release of the drug from the formulated patches was studied using the USP dissolution apparatus, and the results indicated that HEC, HPC and chitosan showed the lowest drug release [70%, 76%, and 81%, respectively] while gelatin] sodium alginate and Na CMC gave the highest release [nearly 100%]. Permeation of larnoxicam formulated in different patches through rabbit buccal mucosa was also studied and the results showed that gelatin and chitosan patches resulted in the highest drug permeation. Kinetics of drug release from the different patches was found to follow zero order or diffusion kinetics

Mycotic vulvovaginitis: epidemiology, pathogenesis and profile of antifungal agents

VulvoVaginitis is the most common gynecological problem affecting millions of women world wide. At some point in their life time, nearly 75% of all women experience an attack of Candida Vulvovaginitis. Little is known about the prevalence of different causes of Vulvovaginitis and risk factors for this entity in Saudi Arabia. This survey was conducted to study the etiologic agents associated with mycotic Vulvovaginitis and review some predisposing factors correlated with this type of infection in Al -Madina Al- Munawarah, Saudi Arabia. High vaginal swabs [HVS] specimens were collected from 1000 patients attending gynecological out patients clinics of two general hospitals in Al-Madinah Al-Munawarah. Specimens were cultured on specific medium for yeasts and identification of the positive isolates was carried out using "API" kit. Antifungal sensitivity pattern of the isolates was tested out using "Candifast" kit. Proteolytic enzyme activity of the isolates was also detected. Three hundred and forty nine positive cases of yeast infection out of 1000 diagnosed cases representing 34.9% were recorded in this study. These positive cases were classified on the basis of the risk factor as; diabetic [28.9%]; pregnant, [32.1%]; pregnant and diabetic [7.5%]; Menopause [5.5%]; oral contraceptive users [10.6%]; post hysterectomy [1.4%] and no observed factor in 14% of the cases. Twenty one different species belonging to 7 genera were recovered in this study. The genus Candida was the most common [93.4%] and included 14 different species. Candida albicans was the highest in prevalence [51.3%]. The non-Candida species were Saccharomyces cervisiae [2.9%]; Rhodotorula rubra [1.1%]; R. minuta [0.9%] Debaryomyces hansenii [0.6%]; Trichosporon mucoides [0.6%]; Cryptococcus neoformans [0.3%] and Pichia ohmeri [0.3%]. Most of the Candida species were sensitive towards nystatin, amphoterian B and fluconazole and resistant to other azole drugs. Saccharomyces cervisiae and Debaryomyces hansenii were sensitive to almost all the tested antifungal drugs.The rest of the species were variable in their pattern. Proteolytic activity of C. albicans reached its maximum value after 72 hours. Neutral proteases was the highest at pH 6.5 followed by alkaline proteases at pH 8.2 and the least amount was acid protease at pH 3.5. The results of this survey which is the first study done in this region threw some light on the prevalence, etiology, sensitivity profile of the etiologic agents and the risk factors of Vulvovaginitis in Al-Madina Al-Munawarah Saudi Arabia. Awareness towards the increase incidence of Vulvovaginits needs more attention to be paid for fungal infection and antif ungal sensitivity

Formulation of ketorolac tromethamine in semi-solid dosage forms

Ketorolac tromethamine [KT] is one of NSAIDs that has GIT, renal and hepatic disorder if taken orally. The study aimed at avoiding the adverse effects of KT by formulating it in different topical dosage form such as gel [Sodium aignate, NaCMC, HPMC, Carbopol 934 and Pluronic F127], emulgel [O/W], microemulsion and cream [O/Wand W/O]. The interactions between KT, polymers and other ingredients used were studied using differential scanning calorimeter [DSC] and Infra red [JR] spectroscopy. The physical properties of these formulations appearance, homogeneity, pH and viscosity were studied The in-vitro release of KT from these formulations through cellophane membrane was carried out. The kinetic study of KT release from these formulations was also studied In-vitro study of KT permeation in diffusion cell using rat skin from the selected formulations was carried out. Physical investigation of KT and polymers indicated that no interaction between KT and polymers. Among the polymers used in gel formulations, HPMC and NaCMC gave the highest release rate of KT in-vitro, while pluronic F127 gave promising sustained release, In case of emulgel formulations, O/W emulgel base gave higher release than microemulsion base, Also in case of emulsion ointment base formulations, the release of KT from 0/W base was higher than W/0 type which gave the lowest release. In-vitro study of KT through the diffusion cell using rat skin as biological membrane, higher permeation was obtained in case of carbopol 934 gel and O/W emulgel comparison with pluronic F127 gel which gave the lowest permeation of KT

Clinical evaluation of oral insulin formulation in type-2 diabetic patients

The objective of this study was to assess the clinical efficacy of a single dose of insulin [100 IU] incorporated with a group of additives in enteric-coated, chitosan-coated capsules through its glucose lowering effect over a period of 12 hours. The capsules were administered orally to type-2 diabetic patients. The results were compared to those of oral administration of capsules of the same coating containing only insulin [100 IU] without additives, S.C. insulin injection [average dose 18 IU] and oral placebo. Ten patients with type-2 diabetes were enrolled in this blind, placebo-controlled, four-way crossover study. It was found that, capsules containing, only insulin resulted in a slight decrease in the mean blood glucose levels of the 10 patients compared to control especially in the period from 6 to 12 hours following administration. On the other hand, capsules containing insulin with additives showed a remarkable lowering of the blood glucose levels. Their effect started 3 hours following administration and sustained to the end of the experiment [12 h]. During the first 4 hours following administration was the reduction resulting from S.C. insulin was significantly higher than that produced by capsules containing insulin with additives. In the period from 4-7 hours, the effect of the capsules was comparable to that of S.C. insulin [no significant difference]. Beyond that [7-12 hours], there was a highly significant difference in favor of capsules. The relative bioavailability obtained by capsules containing only insulin was 3.43%, while that obtained by capsules containing insulin with additives was 18.54%

Detection of cancer of pancreas by native fluorescence of blood components: a preliminary report

Cancer of pancreas is one of the major concerns in health care. Since the early detection of tumour is essential for effective disease management, many methods such as ultrasound, computed tomography [CT] or magnetic resonance image [MRI] scans, etc., are used. Our goal in this work is to develop a new technique of optical diagnosis for detection of cancer of pancreas. In this study we analyzed the blood components through fluorescence emission and synchronous spectroscopic techniques to distinguish features of cancer of pancreas. The sample consisted of 20 patients with cancer and 80 healthy subjects. Extracts of formed elements and plasma of pancreatic cancer patients showed unmistakable features distinct from those of healthy subjects, mainly because of high concentration of porphyrin and bilirubin fluorophores in blood [P<0.001]. In conclusion this preliminary study showed that through optical diagnosis based on fluorescence emission and synchronous spectra, it is possible to detect pancreatic cancer. This is a newly emerging, non-invasive and reliable technique for early detection of cancer